LLY-283

Catalog No.S8883 Batch:S888302

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Technical Data

Formula

C17H18N4O4
Molecular Weight 342.35 CAS No. 2040291-27-6
Solubility (25°C)* In vitro DMSO 68 mg/mL (198.62 mM)
Water 8 mg/mL (23.36 mM)
Ethanol 2 mg/mL (5.84 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity.
Targets
PRMT5 [1]
(Cell-free assay)		 PRMT5 [1]
(Cell-based assay)
22 nM 25 nM
In vitro

LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 ± 3 and 25 ± 1 nM, respectively. LLY-283 directly binds to and occupies the SAM pocket. LLY-283 is a low nanomolar enzymatic inhibitor of the PRMT5:MEP50 complex in biochemical assays and is selective for PRMT5 over other methyltransferases including related family members.[1]
In vivo LLY-283 shows antitumor activity in mouse xenografts when dosed orally and can serves as an excellent probe molecule for understanding the biological function of PRMT5 in normal and cancer cells. LLY-283 can be used as an in vivo tool compound to evaluate the pharmacology of PRMT5 inhibition.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Sf9 cells, A375 tumor cells, MCF7 cells

  • Concentrations

    1 µM, 10 µM

  • Incubation Time

    48 h

  • Method

    PRMT5 cellular assay. MCF7 cells are grown in DMEM supplemented with 10% FBS, penicillin (100 units/ml) and streptomycin (100 µg/ml). 40% confluent cells are treated with different concentrations of LLY-283 or DMSO control for 48 h. The levels of SmBB' and symmetrically dimethylated SmBB' are analyzed in westernblot.
Animal Study:

[1]
  • Animal Models

    SCID mice with A375 derived xenografts

  • Dosages

    20 mg/kg

  • Administration

    Oral gavage

Selleck's LLY-283 has been cited by 4 publications

Long non-coding RNA-derived peptides are immunogenic and drive a potent anti-tumour response [ Nat Commun, 2023, 14(1):1078] PubMed: 36841868
Inhibition of histone methyltransferase PRMT5 attenuates cisplatin-induced hearing loss through the PI3K/Akt-mediated mitochondrial apoptotic pathway [ J Pharm Anal, 2023, 13(6):590-602] PubMed: 37440906
A PRMT5 inhibitor protects against noise-induced hearing loss by alleviating ROS accumulation [ Ecotoxicol Environ Saf, 2022, 243:113992] PubMed: 35994911
Explore the effect of LLY-283 on the ototoxicity of auditory cells caused by cisplatin: A bioinformatic analysis based on RNA-seq [ J Clin Lab Anal, 2022, e24176] PubMed: 34997776

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.